Enhanced G-protein coupled receptors-mediated contraction and reduced endothelium-dependent relaxation in hypertension

Research output: Contribution to journalArticle


The present study was designed to demonstrate a hypothesis that some G-protein coupled receptors are up-regulated and a dysfunction of endothelium occurs in hypertension. The arteries from hypertensive patients and spontaneously hypertensive rats (SHR) were tested. An in vitro myograph system was used to obtain concentration-contraction curves mediated by endothelin ETA, endothelin ETB, 5-hydroxytryptamine 2A (5HT(2A))-receptors and alpha(1)-adrenoceptors in the arterial segments. In hypertensive patients, the maximum contractions (E-max) induced by endothelin ETB, endothelin ETA and 5-HT receptors were significantly increased with elevated pEC(50) values, while a significantly leftward shift of alpha(1)-adrenoceptor-mediated contraction was seen. Similar results were obtained in SHR. Specific antagonists for 5-HT2A receptors or alpha(1)-adrenoceptors rightward shifted the concentration-contractile curves induced by 5-HT or noradrenalin, while the Emax were not significantly altered, suggesting that the contractions were mediated by 5-HT2A receptors and ocl-adrenoceptors, respectively. Endothelium-dependent maximum relaxation (R-max) in the arterial segments induced by acetylcholine was significantly decreased in both hypertensive patients and SHR. In addition, nitric oxide- and endothelium-derived hyperpolarizing factor-mediated dilatations were decreased significantly and the arterial enclothelial cells were in part lost in SHR. In conclusion, endotheliD ETB, endothelin ETA, 5-HT2A receptor- and alpha-adrenoceptor-mediated contractions were increased in hypertension, while the endotheliurn and its ftinctions were damaged. (c) 2006 Elsevier B.V All rights reserved.


  • He Li
  • Yong-Xiao Cao
  • Hao Liu
  • Cang-Bao Xu
Research areas and keywords

Subject classification (UKÄ) – MANDATORY

  • Pharmacology and Toxicology


  • endothelin receptor, 5-HT receptor, endothelium, alpha(1)-adrenoceptor, hypertension
Original languageEnglish
Pages (from-to)186-194
JournalEuropean Journal of Pharmacology
Issue number2-3
Publication statusPublished - 2007
Publication categoryResearch